Skin is the largest organ of the body and separates the inside of the body from the outside world. It serves several important functions including protecting the body from microorganisms that can cause infections, sensing the outside world, regulating body temperature and maintaining homeostasis of the organism.
Conditions that irritate, clog or inflame the skin can cause symptoms such as redness, swelling, burning and itching. Allergies, irritants, genetic makeup and certain to diseases and immune system problems can cause various skin disorders. New topical formulations are required to treat skin disorders.
U.S. Pat. No. 4,619,916 to Di Stazio discloses 13 tripeptides of the formula pGLU—X-TRP, where pGLU is cyclized glutamic acid (pyroglutamic acid) and X may be GLY, VAL, GLU, ASP, SER, ALA, ASN, GLN, ILE, LEU, PRO, LYS and ARG. Also disclosed are a process for their preparation, pharmaceutical formulations containing them for oral or parenteral administration and their use as hypotensive and analgesic therapeutic agents. Further disclosed are lower alkyl esters of the tryptophan residue, in particular methyl or ethyl esters, for use as protecting groups in the production of the peptides. The protecting groups are removed at the completion of the synthesis process. There is no disclosure of a topical formulation.
WO 92/19254 discloses α-substituted mono, di, tri, tetra and pentapeptides useful in treating obesity, anxiety, gastrointestinal ulcers, pain, stroke and inflammation. Peptides of the formula pGLU—X-TRP are not disclosed.
WO 1999/036078 discloses a substantially non-toxic fraction isolated from the venom of the snake Vipera xanthina which fraction has an analgesic effect. Also described are a pharmaceutical composition for use as an analgesic comprising the non-toxic fraction, and a method for the relief of pain comprising administrating the non-toxic fraction.
WO2001/003710 discloses a substantially non-toxic fraction isolated from venom of several snake species, which fraction has an analgesic effect. The fraction has the characteristics of a fraction from snake venom purified on a Mono Q ion exchange column. Also described is a pharmaceutical composition for use as an analgesic comprising the non-toxic fraction, and a method for the relief of pain comprising administrating the non-toxic fraction.
WO2002012269 discloses a pharmaceutical composition for topical administration comprising an analgesic effective amount of a peptide comprising L-amino acids of the formula (I): pGLU—X—Y—Z (I) and a pharmaceutically acceptable excipient. X is an amino acid selected from the group consisting of GLY, VAL, GLU, ASP, SER, ALA, ASN, GLN, ILE, LEU, PRO, LYS and ARG, Y is TRP or THR, and Z is any L-amino acid, or Z is null. When Z is any L-amino acid, one but not both of Y and Z is TRP, and when Z is null, Y=TRP. An alkyl group may be attached to an amino acid of the peptide. Also disclosed are the peptide, the preparation of the pharmaceutical composition and a topical method of treating or preventing pain in a mammal.